(NZ)-N-(2-bicyclo[3.3.1]nonanylidene)hydroxylamine

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: (NZ)-N-(2-bicyclo[3.3.1]nonanylidene)hydroxylamine
• 化学式: C₉H₁₅NO
• 分子量: 153.22
• InChiKey: JQFMMZYYTWZDBQ-KTKRTIGZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.89
• 拓扑面积：
  32.6
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• [EN] ADAMANTYL ACETAMIDES AS HYDROXYSTEROID DEHYDROGENASE INHIBITORS<br/>[FR] ADAMANTYL ACETAMIDES UTILISES COMME INHIBITEURS DE LA HYDROXYSTEROIDE DESHYDROGENASE
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2004056744A1

  公开（公告）日：2004-07-08

  formulae (I)the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n represents an integer being 1 or 2; R1 and R2 each independently represents hydrogen C1-4alkyl, NR9R10, C1-4alkyloxy; or R1 and R2 taken together with the carbon atom with which they are attached form a C3-6cycloalkyl; and where n is 2, either R1 or R2 may be absent to form an unsaturated bond; R3 represents a C6-12cycloalkyl, preferably selected from cylo-octanyl and cyclohexyl or R3 represents a monovalent radical having one of the following formulae(a) (b) (c) (l) (q) (r) (g) (u) (o) (w) (j) (k) (t) wherein said C6-12cycloalkyl or monovalent radical may optionally be substituted with one, or where possible two, three or more substituents selected from the group consisting of C1-4alkyl, C1-4alkyloxy, halo or hydroxy; Q represents Het1 or Ar2 wherein said C3-8cycloalkyl, Het1 or Ar2 are optionally substituted with one or where possible two or more substituents selected from halo, C1-4alkyl, C1-4alkyloxy, hydroxy, nitro, NR5R6, C1-4alkyloxy substituted with one or where possible two, three or more substituents each independently selected from hydroxycarbonyl, Het2 and NR7R8, and C1-4alkyl substituted with one or where possible two or three halo substituents, preferably trifluoromethyl; R5 and R6 each independently represent hydrogen, C1-4alkyl, or C1-4alkyl substituted with phenyl; R7 and R8 each independently represent hydrogen or C1-4alkyl; R9 and R10? each independently represent hydrogen, C1-4alkyl or C1-4alkyloxycarbonyl; L represents C1-4alkyl; Het1 represents a heterocycle selected from pyridinyl, thiophenyl, or 1,3-benzodioxolyl; Het2 represents piperidinyl, pyrrolidinyl or morpholinyl; Ar2 represents phenyl, naphtyl or indenyl.

  公式（I）N-氧化物形式，其药学上可接受的加盐和立体化学异构体形式，其中n表示整数1或2；R1和R2分别表示氢C1-4烷基，NR9R10，C1-4烷氧基；或者R1和R2与它们连接的碳原子一起形成C3-6环烷基；当n为2时，R1或R2中的任一者可以缺失以形成不饱和键；R3表示C6-12环烷基，优选选择自环辛基和环己基，或者R3表示具有以下公式之一的一价基团（a）（b）（c）（l）（q）（r）（g）（u）（o）（w）（j）（k）（t），其中所述C6-12环烷基或一价基团可以选择性地用来自C1-4烷基，C1-4烷氧基，卤素或羟基的一个，或可能是两个，三个或更多个取代基取代；Q表示Het1或Ar2，其中所述C3-8环烷基，Het1或Ar2可以选择性地用来自卤素，C1-4烷基，C1-4烷氧基，羟基，硝基，NR5R6，C1-4烷氧基的一个，或可能是两个，三个或更多个取代基，每个独立选自羟基羰基，Het2和NR7R8，以及C1-4烷基的一个，或可能是两个或三个卤素取代基，优选三氟甲基；R5和R6各自独立地表示氢，C1-4烷基，或用苯基取代的C1-4烷基；R7和R8各自独立地表示氢或C1-4烷基；R9和R10各自独立地表示氢，C1-4烷基或C1-4烷氧羰基；L表示C1-4烷基；Het1表示从吡啶基，噻吩基或1,3-苯并二氧杂环烷中选择的杂环；Het2表示哌啶基，吡咯烷基或吗啉基；Ar2表示苯基，萘基或茚基。
• Adamantyl acetamides as 11-beta hydroxysteroid dehydrogenase inhibitors
  申请人：Linders Theodorus Maria Joannes

  公开号：US20060079506A1

  公开（公告）日：2006-04-13

  the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n represents an integer being 1 or 2; R 1 and R 2 each independently represents hydrogen C 1-4 alkyl, NR 9 R 10 , C 1-4 alkyloxy; or R 1 and R 2 taken together with the carbon atom with which they are attached form a C 3-6 cycloalkyl; and where n is 2, either R 1 or R 2 may be absent to form an unsaturated bond; R 3 represents a C 6-12 cycloalkyl, preferably selected from cylo-octanyl and cyclohexyl or R 3 represents a monovalent radical having one of the following formulae wherein said C 6-12 cycloalkyl or monovalent radical may optionally be substituted with one, or where possible two, three or more substituents selected from the group consisting of C 1-4 alkyl, C 1-4 alkyloxy, halo or hydroxy; Q represents Het 1 or Ar 2 wherein said C 3-8 cycloalkyl, Het 1 or Ar 2 are optionally substituted with one or where possible two or more substituents selected from halo, C 1-4 alkyl, C 1-4 alkyloxy, hydroxy, nitro, NR 5 R 6 , C 1-4 alkyloxy substituted with one or where possible two, three or more substituents each independently selected from hydroxycarbonyl, Het 2 and NR 7 R 8 , and C 1-4 alkyl substituted with one or where possible two or three halo substituents, preferably trifluoromethyl; R 5 and R 6 each independently represent hydrogen, C 1-4 alkyl, or C 1-4 alkyl substituted with phenyl; R 7 and R 8 each independently represent hydrogen or C 1-4 alkyl; R 9 and R 10 each independently represent hydrogen, C 1-4 alkyl or C 1-4 alkyloxycarbonyl; L represents C 1-4 alkyl; Het 1 represents a heterocycle selected from pyridinyl, thiophenyl, or 1,3-benzodioxolyl; Het 2 represents piperidinyl, pyrrolidinyl or morpholinyl; Ar 2 represents phenyl, naphtyl or indenyl.

  N-氧化物形式，其药学上可接受的加合盐以及立体化学异构体形式，其中n表示1或2的整数；R1和R2各自独立地表示氢C1-4烷基，NR9R10，C1-4烷氧基; 或者R1和R2与它们附着的碳原子一起形成C3-6环烷基; 当n为2时，R1或R2中的任一可以不存在以形成不饱和键; R3表示C6-12环烷基，优选从环辛基和环己基中选择，或者R3表示具有以下式子之一的单价基团，其中所述的C6-12环烷基或单价基团可以选择地被一个、或可能两个、三个或更多来自C1-4烷基，C1-4烷氧基，卤素或羟基的取代基所取代; Q表示Het1或Ar2，其中所述的C3-8环烷基，Het1或Ar2可以选择地被一个或可能两个或更多来自卤素，C1-4烷基，C1-4烷氧基，羟基，硝基，NR5R6，C1-4烷氧基取代，其中每个独立地选择自羟基羰基，Het2和NR7R8，以及C1-4烷基取代，其中每个独立地选择自三氟甲基等卤素取代基; R5和R6各自独立地表示氢，C1-4烷基，或C1-4烷基取代苯基; R7和R8各自独立地表示氢或C1-4烷基; R9和R10各自独立地表示氢，C1-4烷基或C1-4烷氧羰基; L表示C1-4烷基; Het1表示从吡啶基，噻吩基或1,3-苯并二氧杂环中选择的杂环; Het2表示哌啶基，吡咯烷基或吗啉基; Ar2表示苯基，萘基或茚基。
• ADAMANTYL ACETAMIDES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS
  申请人：JANSSEN PHARMACEUTICA N.V.

  公开号：EP1581476A2

  公开（公告）日：2005-10-05
• AMIDES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS
  申请人：Janssen Pharmaceutica NV

  公开号：EP1581476B1

  公开（公告）日：2016-11-16
• US7332524B2
  申请人：——

  公开号：US7332524B2

  公开（公告）日：2008-02-19